期刊
MOLECULES
卷 26, 期 13, 页码 -出版社
MDPI
DOI: 10.3390/molecules26133821
关键词
HIV-RT; ribonuclease H; dual inhibitors; docking; putative binding
资金
- Regione Autonoma della Sardegna (RAS) [RASSR17032]
Current therapy for HIV infection involves a combination of antiretroviral drugs to reduce the selection of resistant mutants. A study has investigated potential multi-target agents for anti-HIV treatment, with a compound showing the most potent inhibition against certain functions of HIV reverse transcriptase.
Current therapeutic protocols for the treatment of HIV infection consist of the combination of diverse anti-retroviral drugs in order to reduce the selection of resistant mutants and to allow for the use of lower doses of each single agent to reduce toxicity. However, avoiding drugs interactions and patient compliance are issues not fully accomplished so far. Pursuing on our investigation on potential anti HIV multi-target agents we have designed and synthesized a small library of biphenylhydrazo 4-arylthiazoles derivatives and evaluated to investigate the ability of the new derivatives to simultaneously inhibit both associated functions of HIV reverse transcriptase. All compounds were active towards the two functions, although at different concentrations. The substitution pattern on the biphenyl moiety appears relevant to determine the activity. In particular, compound 2-{3-[(2-{4-[4-(hydroxynitroso)phenyl]-1,3-thiazol-2-yl} hydrazin-1-ylidene) methyl]-4-methoxyphenyl} benzamide bromide (EMAC2063) was the most potent towards RNaseH (IC50 = 4.5 mM)- and RDDP (IC50 = 8.0 mM) HIV RT-associated functions.
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